CHEMBL1778208 (CID 53248730) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(23)
 
 
Inconclusive(1)
 
 
Unspecified(16)
 
 
Top Targets:
CAP ED(3)
 
 
 
BioAssay Types:
Literature(40)
 
 
 
 
BioActivity Types:
IC50(18)
 
 
 
 
EC50(3)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 40    Data Row: 40   Total Pages: 1   
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID131279432]
IC50 0.022Antiproliferative activity against human KB cells [AID597831, Type: Literature]
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2
[SID131279432]
IC50 0.023Antiproliferative activity against human A375 cells [AID597823, Type: Literature]
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3
[SID131279432]
IC50 0.023Antiproliferative activity against human BT474 cells [AID597824, Type: Literature]
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4
[SID131279432]
IC50 0.023Antiproliferative activity against human A549 cells [AID597826, Type: Literature]
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5
[SID131279432]
IC50 0.042Antiproliferative activity against human T98G cells [AID597829, Type: Literature]
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6
[SID131279432]
IC50 0.045Antiproliferative activity against human DU145 cells [AID597828, Type: Literature]
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7
[SID131279432]
IC50 0.047Antiproliferative activity against human NCI-H1975 cells [AID597889, Type: Literature]
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8
[SID131279432]
IC50 0.049Antiproliferative activity against human KB 8.5 cells [AID597832, Type: Literature]
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9
[SID131279432]
EC50 0.056Antiproliferative activity against human HCT116 cells [AID597820, Type: Literature]
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10
[SID131279432]
EC50 0.056Antiproliferative activity against human HCT116 cells by luminescence assay [AID598613, Type: Literature]
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11
[SID131279432]
IC50 0.079Inhibition of v-Src by cell-based functional assay [AID598612, Type: Literature]
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12
[SID131279432]
IC50 0.079Inhibition of HSP90 in human HCT-116 cells expressing V-Src-firefly luciferase fusion protein after 3 to 6 hrs [AID597819, Type: Literature]
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13
[SID131279432]
IC50 0.08Antiproliferative activity against human U87MG cells [AID597830, Type: Literature]
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14
[SID131279432]
EC50 0.08Antiproliferative activity against human U87 cells by luminescence assay [AID598614, Type: Literature]
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15
[SID131279432]
IC50 0.082Inhibition of HSP90alpha after 3 hrs by fluorescence polarization binding assay [AID598611, Type: Literature]
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16
[SID131279432]
IC50 0.082Inhibition of HSP90 by fluorescence polarization assay [AID597818, Type: Literature]
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17
[SID131279432]
IC50 0.092Antiproliferative activity against human WM266.4 cells [AID597825, Type: Literature]
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18
[SID131279432]
IC50 0.111Antiproliferative activity against human MDA-MB-361 cells [AID597827, Type: Literature]
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19
[SID131279432]
 Binding affinity to N-terminal HSP90 ATP-binding site by X-ray crystallography [AID597836, Type: Literature]
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20
[SID131279432]
 Upregulation of HSP90 expression in human MDA-MB-361 xenograft in vivo model at 50 m/kg, po measured after 6 hrs post dose [AID597885, Type: Literature]
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21
[SID131279432]
 Upregulation of HSP70 expression in human MDA-MB-361 xenograft in vivo model at 50 m/kg, po measured after 6 hrs post dose [AID597886, Type: Literature]
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22
[SID131279432]
 Downregulation of HER2 expression in human MDA-MB-361 xenograft in vivo model at 50 m/kg, po measured after 6 hrs post dose [AID597887, Type: Literature]
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23
[SID131279432]
 Downregulation of phosphorylated AKT in human MDA-MB-361 xenograft in vivo model at 50 m/kg, po measured after 6 hrs post dose [AID597888, Type: Literature]
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24
[SID131279432]
IC50 1Antiproliferative activity against P-gp overexpressing human KBV1 cells [AID597833, Type: Literature]
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25
[SID131279432]
IC50 33Inhibition of human ERG by patch clamp method [AID597834, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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26
[SID131279432]
IC50 33Inhibition of human ERG by patch clamp method [AID597834, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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27
[SID131279432]
IC50 33Inhibition of human ERG by patch clamp method [AID597834, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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28
[SID131279432]
IC50 33Inhibition of human ERG by patch clamp method [AID597834, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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29
[SID131279432]
IC50 33Inhibition of human ERG by patch clamp method [AID597834, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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30
[SID131279432]
 Inhibition of human ERG at 11 uM by patch clamp method [AID597835, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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31
[SID131279432]
 Inhibition of human ERG at 11 uM by patch clamp method [AID597835, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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32
[SID131279432]
 Inhibition of human ERG at 11 uM by patch clamp method [AID597835, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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33
[SID131279432]
 Inhibition of human ERG at 11 uM by patch clamp method [AID597835, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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34
[SID131279432]
 Inhibition of human ERG at 11 uM by patch clamp method [AID597835, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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35
[SID131279432]
 Plasma concentration human MDA-MB-361 xenograft in vivo model at 50 mg/kg, po measured at 6 hrs post dose [AID597837, Type: Literature]
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36
[SID131279432]
 Drug level in tumor of human MDA-MB-361 xenograft in vivo model at 50 mg/kg, po measured at 6 hrs post dose [AID597838, Type: Literature]
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37
[SID131279432]
 Plasma concentration in human MDA-MB-361 xenograft in vivo model at 50 mg/kg, po measured at 24 hrs post dose [AID597839, Type: Literature]
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38
[SID131279432]
 Drug level in tumor of human MDA-MB-361 xenograft in vivo model at 50 mg/kg, po measured at 24 hrs post dose [AID597884, Type: Literature]
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39
[SID131279432]
 Half life in human liver microsomes [AID598619, Type: Literature]
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40
[SID131279432]
 Half life in mouse liver microsomes [AID598620, Type: Literature]
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41
[SID131279432]
 Half life in rat liver microsomes [AID598621, Type: Literature]
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42
[SID131279432]
 Half life in rat liver microsomes [AID597821, Type: Literature]
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43
[SID131279432]
 Solubility of the compound [AID597822, Type: Literature]
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44
[SID131279432]
 Inhibition of CYP2C9 at 3 uM [AID598615, Type: Literature]
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45
[SID131279432]
 Inhibition of CYP2D6 at 3 uM [AID598616, Type: Literature]
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46
[SID131279432]
 Inhibition of CYP3A4 at 3 uM [AID598617, Type: Literature]
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47
[SID131279432]
 Aqueous solubility of the compound [AID598618, Type: Literature]
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48
[SID131279432]
IC50 Inhibition of human ERG by HT patch clamp assay [AID598622, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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49
[SID131279432]
IC50 Inhibition of human ERG by HT patch clamp assay [AID598622, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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50
[SID131279432]
IC50 Inhibition of human ERG by HT patch clamp assay [AID598622, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
View